Therapeutic potential of chalcone-1,2,3-triazole hybrids as anti-tumour agents: a systematic review and SAR studies.

Abstract

The study of chalcone-1,2,3-triazole hybrids for anticancer activity is quite a recent area of focus, primarily because of the increasing demand for developing new drugs to treat cancer. The chalcones and 1,2,3-triazole rings in hybrid compounds has recently emerged as a promising strategy for developing novel anticancer agents. The 1,2,3-triazole ring, known for its stability and hydrogen bonding capabilities, enhances the target binding affinity of these hybrids. Chalcones possess an α,β-unsaturated carbonyl system crucial for their anticancer activity The synergistic effect of these two moieties results in compounds with potent anticancer properties. This review explores the structure-activity relationship studies which revealed that the electronic and lipophilic properties of substituents on the phenyl rings of chalcones significantly influence their anticancer activity. Electron-donating and electron-withdrawing groups can affect cellular uptake and target engagement. Incorporating various substituents into the 1,2,3-triazole ring can improve selectivity and potency against specific cancer cell lines. These hybrids often exert their anticancer effects through apoptosis and cell cycle disruption. Recent research indicates 1,2,3-triazole chalcone hybrids hold therapeutic promise as anticancer agents. Further optimization through SAR studies and in-depth mechanistic investigations could lead to the development of highly potent and selective anticancer agents with minimal toxicity.